Covalent modifiers: an orthogonal approach to drug design.
about
Fine-tuning multiprotein complexes using small moleculesThe pharmacological landscape and therapeutic potential of serine hydrolasesFeatures of protein-protein interactions that translate into potent inhibitors: topology, surface area and affinityDeveloping irreversible inhibitors of the protein kinase cysteinomeStructural Framework for Covalent Inhibition of Clostridium botulinum Neurotoxin A by Targeting Cys165Electrophilic Fragment-Based Design of Reversible Covalent Kinase InhibitorsReversible targeting of noncatalytic cysteines with chemically tuned electrophilesCovalent docking of large libraries for the discovery of chemical probesMining a cathepsin inhibitor library for new antiparasitic drug leadsSynthetic and Biological Studies of Sesquiterpene Polygodial: Activity of 9-Epipolygodial against Drug-Resistant Cancer CellsCovalent Modifiers: A Chemical Perspective on the Reactivity of α,β-Unsaturated Carbonyls with Thiols via Hetero-Michael Addition ReactionsHigh-throughput screening for growth inhibitors using a yeast model of familial paraganglioma.Design, Synthesis, and Biological Evaluation of Novel Conformationally Constrained Inhibitors Targeting EGFR.Benzylidene cyclopentenediones: First irreversible inhibitors against botulinum neurotoxin A's zinc endopeptidase.Structure-activity relationships of a small-molecule inhibitor of the PDZ domain of PICK1Transitioning pharmacoperones to therapeutic use: in vivo proof-of-principle and design of high throughput screens.Chemical methodology as a source of small-molecule checkpoint inhibitors and heat shock protein 70 (Hsp70) modulators.Strategies for discovering and derisking covalent, irreversible enzyme inhibitors.Catalytic reaction mechanism of acetylcholinesterase determined by Born-Oppenheimer ab initio QM/MM molecular dynamics simulations.A road map to evaluate the proteome-wide selectivity of covalent kinase inhibitors.Design of reversible, cysteine-targeted Michael acceptors guided by kinetic and computational analysis.Design and pharmacological characterization of VUF14480, a covalent partial agonist that interacts with cysteine 98(3.36) of the human histamine H₄ receptor.Covalent small molecule inhibitors of Ca(2+)-bound S100B.A genetically encoded aza-Michael acceptor for covalent cross-linking of protein-receptor complexes.Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation.Synthesis of sesquiterpene-inspired derivatives designed for covalent binding and their inhibition of the NF-κB pathway.Bruton's TK inhibitors: structural insights and evolution of clinical candidates.An allenic Pauson-Khand approach to 6,12-guaianolides.Mapping proteome-wide interactions of reactive chemicals using chemoproteomic platforms.Modular Synthesis of Novel Macrocycles Bearing α,β-Unsaturated Chemotypes through a Series of One-Pot, Sequential Protocols.Identification of selective covalent inhibitors of platelet activating factor acetylhydrolase 1B2 from the screening of an oxadiazolone-capped peptoid-azapeptoid hybrid library.Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) InhibitorsReduction of oxidative stress and inflammation by blunting daily acute glucose fluctuations in patients with type 2 diabetes: role of dipeptidyl peptidase-IV inhibition.A novel 2,5-diaminopyrimidine-based affinity probe for Bruton's tyrosine kinase.Monocarbonyl analogs of curcumin inhibit growth of antibiotic sensitive and resistant strains of Mycobacterium tuberculosis.Arylfluorosulfates Inactivate Intracellular Lipid Binding Protein(s) through Chemoselective SuFEx Reaction with a Binding Site Tyr ResidueSynthesis of piperlogs and analysis of their effects on cellsClinical evidence and mechanistic basis for vildagliptin's action when added to metformin.From conventional to unusual enzyme inhibitor scaffolds: the quest for target specificity.Mechanisms of action of the dipeptidyl peptidase-4 inhibitor vildagliptin in humans.
P2860
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P2860
Covalent modifiers: an orthogonal approach to drug design.
description
2009 nî lūn-bûn
@nan
2009 թուականի Մարտին հրատարակուած գիտական յօդուած
@hyw
2009 թվականի մարտին հրատարակված գիտական հոդված
@hy
2009年の論文
@ja
2009年論文
@yue
2009年論文
@zh-hant
2009年論文
@zh-hk
2009年論文
@zh-mo
2009年論文
@zh-tw
2009年论文
@wuu
name
Covalent modifiers: an orthogonal approach to drug design.
@ast
Covalent modifiers: an orthogonal approach to drug design.
@en
type
label
Covalent modifiers: an orthogonal approach to drug design.
@ast
Covalent modifiers: an orthogonal approach to drug design.
@en
prefLabel
Covalent modifiers: an orthogonal approach to drug design.
@ast
Covalent modifiers: an orthogonal approach to drug design.
@en
P356
P1476
Covalent modifiers: an orthogonal approach to drug design.
@en
P2093
Mark E Duggan
Michele H Potashman
P304
P356
10.1021/JM8008597
P407
P577
2009-03-01T00:00:00Z